In vitro skin absorption and metabolism of benzoic acid, p-aminobenzoic acid, and benzocaine in the hairless guinea pig.
The percutaneous absorption and metabolism of three structurally related compounds, benzoic acid, p-aminobenzoic acid (PABA), and ethyl aminobenzoate (benzocaine), were determined in vitro through hairless guinea pig skin. Benzocaine was also studied in human skin. Absorption of benzocaine was rapid and similar through both viable and nonviable skin. The absorption of the two acidic compounds, benzoic acid and PABA, was greater through nonviable skin. A small portion (6.9%) of absorbed benzoic acid was conjugated with glycine to form hippuric acid. Although N-acetyl-benzocaine had not been observed as a metabolite of benzocaine when studied by other routes of administration, both PABA and benzocaine were extensively N-acetylated during percutaneous absorption. Thus, the metabolism of these compounds should be considered in an accurate assessment of absorption after topical application.
Nathan
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Division of Toxicological Studies, Food and Drug Administration, Washington, D.C. 20204.
Sakr
A
A
Lichtin
J L
JL
Bronaugh
R L
RL
D010129:4-Aminobenzoic Acid / Q000378:metabolism / Q000493:pharmacokinetics*; D000693:Anaerobiosis; D000818:Animals; D001565:Benzoates / Q000378:metabolism / Q000493:pharmacokinetics*; D001566:Benzocaine / Q000378:metabolism / Q000493:pharmacokinetics*; D019817:Benzoic Acid; D001711:Biotransformation; D002855:Chromatography, Thin Layer; D004058:Diffusion; D005947:Glucose / Q000378:metabolism; D006168:Guinea Pigs; D006801:Humans; D066298:In Vitro Techniques; D012867:Skin / Q000378:metabolism*; D012869:Skin Absorption
D001565:Benzoates; D019817:Benzoic Acid; D005947:Glucose; D010129:4-Aminobenzoic Acid; D001566:Benzocaine